This invention relates generally to an antimicrobial form and more particularly to a medicamentous form for external use with a strong antiexudative, antiphlogistic, and antimicrobial effect in a suitable aqueous or ointment base applicable as an opthalmologic, otolaryngologic, or dermatologic drug.
Arachidic acid is liberated in damaged, wounded, or inflamed tissues from phospholipids of cytoplasmatic membranes by the action of phospholipase enzyme and may be then metabolized by the cyclooxygenase cycle (by cyclooxygenase enzyme) or the lipooxygenase cycle (by lipooxygenase enzyme) to prostanoids and eicosanoids. Antiphlogistics of both the steroid and nonsteroid nature, antibiotics, and sulfonamides are often used for therapeutic purposes. The antibiotics, which specifically suppress pathogenic microbes and are often used in ophthalmology, are tetracycline, chloramphenicol, bacitracin, and neomycin. Therapeutics which prevent the development of inflammation (antiphlogistics) are both steroid and nonsteroid. The steroid antiphlogistics (e.g., dexamethasone) block phospholipase. The antiinflammatory drugs of nonsteroid nature (e.g., indomethacin, flurbiprofen, pirprofen) block cyclooxygenase and others. The blockage of these enzymes is important, because the products formed in metabolic cycles have a strong chemotactic effect (they cause accumulation of leucocytes in the sites of origin), (e.g., some leucotrienes) and increase the vascular permeability. This contributes to an excess development of the inflammation. Inflammations, (both of infectious and noninfectious origin) are very dangerous for the anterior and posterior segments of the eye. Thus, scars formed in the cornea during the final stage of the healing process cause the loss of an exceptional function of this tissue, i.e. transparency. The loss of transparency of optical media of the eye (cornea, lens) then leads to a reduction or even loss of sight.
A disadvantage of locally applied antiphlogistics is the relatively low efficiency, retarded healing, and contribution to the development of infection. The local effect of antibiotics is limited. There is also a danger of development of an allergic reaction. A higher concentration of the antibiotics, which is necessary for obtaining the healing effect in many cases, acts toxically on the tissue. For this reason, local treatment is mostly supplemented with the general administration of antibiotics, which has disastrous consequences with respect to the suppression of antibody formation and the damage to the striking power of organism against infection. To this end, there have been several attempts to provide positive methods of treatment.
One of the very prospective possibilities of treatment is the inhibition of plasmin and other destruction proteases (e.g., collagenase or elastase) with specific inhibitors. These enzymes either directly develop the destruction processes (e.g., plasmin) or enable these processes by their own activity (e.g., collagenase, elastase). However, plasmin is effective not only as an initiator developing the degeneration processes proceeding in cascades, but also contributes to an excessive development of inflammation by several other mechanisms of which at least chemotaxis should be mentioned.
Apart from other methods, plasmin can be inhibited by aprotinin. This substance, when administered in an aqueous solution and low concentrations, has been successfully used in the treatment of some lesions of the anterior segment of the eye. Aprotinin inhibits not only plasmin but also several other proteolytic enzymes (for example, leucocytic elaslase), which contributes to the destruction processes.
What is needed then is a medicamentous form for external use as an opthalmologic, otolaryngologic, and dermatologic drug.
This medicamentous form must have strong antiexudative, antiphlogistic, and antimicrobial effect. This medicamentous form is presenting lacking in the prior art.